BUSPIRONE WITHDRAWAL AND TAPERING HELP

Buspirone is an anti-anxiety agent of the azapirone class of medications that are commonly used as an add-on to antidepressants. Buspirone works by stimulating Serotonin type receptors on nerves, changing the chemical messages that nerves transmit to each other. Buspirone has moderate affinity for brain Dopamine receptors and some studies do suggest that Buspirone has an indirect effect on other neurotransmitter systems. Due to the short half-life of Buspar, multiple daily dosages are generally required.  

Buspirone is approved by the FDA for the treatment of anxiety disorders and short-term relief of anxiety symptoms. In the United Kingdom, Buspirone is indicated only for short-term treatment of anxiety.

Buspirone works by stimulating Serotonin type receptors on nerves, changing the chemical messages that nerves transmit to each other. Buspirone has moderate affinity for brain Dopamine receptors and some studies do suggest that Buspirone has an indirect effect on other neurotransmitter systems. Due to the short half-life of Buspirone , multiple daily dosages are generally required. 

Approximately 10% of patients in the Buspirone premarketing clinical efficacy trials discontinued treatment due to an adverse event including central nervous system disturbances, dizziness, insomnia, gastrointestinal upset, nausea and miscellaneous disturbances. 

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BUSPIRONE WITHDRAWAL SYMPTOMS MAY INCLUDE:

abdominal pains, aching, agoraphobia, anxiety, blurred vision, body vibrations, changes in perception, diarrhea, distended abdomen, feeling of unreality, flu-like symptoms, flatulence, food cravings, hair loss, heart palpitations, heavy limbs, increased allergies, increased sense of smell, insomnia, lethargy, loss of balance, metallic taste, muscle spasms, nightmares, panic attacks, paranoia, persistent & unpleasant memories, severe headaches, shaking, short term memory loss, sore mouth and tongue, sound & light sensitivity, speech difficulties, sweating, suicidal thoughts, tinnitus, unusually sensitive, fear.

BUSPIRONE SIDE EFFECTS MAY INCLUDE: 

dizziness, dry mouth, fatigue, headache, light-headedness, nausea, nervousness, unusual excitement, a anger/hostility, blurred vision, bone aches/pain, confusion, constipation, decreased concentration, depression, diarrhea, fast, fluttery heartbeat, incoordination, muscle pain/aches, numbness, pain or weakness in hands or feet, rapid heartbeat, rash, restlessness, stomach and abdominal upset, sweating/clamminess, tingling or pins and needles, tremor, urinary incontinence, vomiting, and weakness

BUSPIRONE ADVERSE REACTIONS MAY INCLUDE: per PDR 

Severe: seizures, suicidal ideation, bleeding, heart failure, myocardial infarction, bradycardia, cardiomyopath, stroke, serotonin syndrome, angioedema, visual impairment 

Moderate: excitability, hostility, confusion, blurred vision, dysphoria, involuntary movements, akathisia, euphoria, hallucinations, hematoma, edema, elevated hepatic enzymes, dyspnea, hypotension, hypertension, conjunctivitis, dysuria, dysarthria, psychosis, myasthenia, bleeding, leukopenia, thrombocytopenia, eosinophilia, photophobia, ejaculation dysfunction, impotence (erectile dysfunction), chest pain (unspecified), ataxia, pseudoparkinsonism, dystonic reaction, galactorrhea, urinary retention 

Mild: dizziness, drowsiness, nausea, headache, diarrhea, tremor, paresthesias, myalgia, muscle cramps, musculoskeletal pain, arthralgia , flushing, xerosis, pruritus, alopecia, hyperhidrosis, rash, weight gain, hypersalivation, flatulence, anorexia, weight loss, appetite stimulation, hyperventilation, fever, syncope, dysgeusia, parosmia, ocular pruritus, menstrual irregularity, libido increase, libido decrease, increased urinary frequency, malaise, acne vulgaris, epistaxis, hiccups, ocular pain, amenorrhea, nocturia, nasal congestion, tinnitus, insomnia, vertigo, restless legs syndrome (RLS), emotional lability, restlessness, ecchymosis, urticaria, weakness

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According to the FDA:

Potential for Withdrawal Reactions in Sedative/Hypnotic/Anxiolytic Drug- Dependent Patients

Because BuSpar (Buspirone) does not exhibit cross-tolerance with benzodiazepines and other common sedative/hypnotic drugs, it will not block the withdrawal syndrome often seen with cessation of therapy with these drugs. Therefore, before starting therapy with BuSpar, it is advisable to withdraw patients gradually, especially patients who have been using a CNS-depressant drug chronically, from their prior treatment. Rebound or withdrawal symptoms may occur over varying time periods, depending in part on the type of drug, and its effective half-life of elimination.

The syndrome of withdrawal from sedative/hypnotic/anxiolytic drugs can appear as any combination of irritability, anxiety, agitation, insomnia, tremor, abdominal cramps, muscle cramps, vomiting, sweating, flu-like symptoms without fever, and occasionally, even as seizures.

Possible Concerns Related to Buspirone's Binding to Dopamine Receptors

Because buspirone can bind to central dopamine receptors, a question has been raised about its potential to cause acute and chronic changes in dopamine-mediated neurological function (eg, dystonia, pseudo-parkinsonism, akathisia, and tardive dyskinesia). Clinical experience in controlled trials has failed to identify any significant neuroleptic-like activity; however, a syndrome of restlessness, appearing shortly after initiation of treatment, has been reported in some small fraction of buspirone-treated patients. The syndrome may be explained in several ways. For example, buspirone may increase central noradrenergic activity; alternatively, the effect may be attributable to dopaminergic effects (ie, represent akathisia). See ADVERSE REACTIONS: Postmarketing Experience.

Physical and Psychological Dependence

In human and animal studies, buspirone has shown no potential for abuse or diversion and there is no evidence that it causes tolerance, or either physical or psychological dependence. Human volunteers with a history of recreational drug or alcohol usage were studied in two double-blind clinical investigations. None of the subjects were able to distinguish between BuSpar and placebo. By contrast, subjects showed a statistically significant preference for methaqualone and diazepam. Studies in monkeys, mice, and rats have indicated that buspirone lacks potential for abuse.

Following chronic administration in the rat, abrupt withdrawal of buspirone did not result in the loss of body weight commonly observed with substances that cause physical dependency.

Although there is no direct evidence that BuSpar causes physical dependence or drug-seeking behavior, it is difficult to predict from experiments the extent to which a CNS-active drug will be misused, diverted, and/or abused once marketed. Consequently, physicians should carefully evaluate patients for a history of drug abuse and follow such patients closely, observing them for signs of BuSpar misuse or abuse (eg, development of tolerance, incrementation of dose, drug-seeking behavior).

REFERENCES:

https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/018731s051lbl.pdf 

https://www.pdr.net/drug-summary/Buspirone-Hydrochloride-Tablets--USP--5-mg--10-mg--15-mg--30-mg--buspirone-hydrochloride-1524

https://www.ncbi.nlm.nih.gov/books/NBK531477/

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